NE 52-QQ57

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Chemical Structure| 1401728-56-0 同义名 : -
CAS号 : 1401728-56-0
货号 : A1165850
分子式 : C24H28N6O
纯度 : 99%+
分子量 : 416.52
MDL号 : MFCD31813600
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 GPR4, a proton sensing G protein-coupled receptor (GPCR), has been shown to respond to acidic pH by eliciting cAMP via gas signaling and plays a key role in tissue acidosis. NE 52-QQ57 is a selective and orally available GPR4 antagonist with an IC50 value of 70 nM[3]. In HEK293 cells, NE 52-QQ57 effectively blocked GPR4-mediated cAMP accumulation with an IC50 value of 26.8 nM. In HUVEC cells which natively express GPR4, physiological acidification (pH 7.4-7.0) resulted in a cAMP increase by ∼55% which was completely prevented by 1 μM NE 52-QQ57. In unanaesthetised mice and rats, NE 52-QQ57 (20 mg/kg) reduced ventilatory response to 5 and 10% CO2[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.00mL

2.40mL

1.20mL

24.01mL

4.80mL

2.40mL
参考文献

[1]Velcicky J, et al. Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis. J Med Chem. 2017 May 11;60(9):3672-3683.

[2]Hosford PS, et al. CNS distribution, signalling properties and central effects of G-protein coupled receptor 4. Neuropharmacology. 2018 Aug;138:381-392.

[3]Velcicky J, Miltz W, Oberhauser B, Orain D, Vaupel A, Weigand K, Dawson King J, Littlewood-Evans A, Nash M, Feifel R, Loetscher P. Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis. J Med Chem. 2017 May 11;60(9):3672-3683.

[4]Hosford PS, Mosienko V, Kishi K, Jurisic G, Seuwen K, Kinzel B, Ludwig MG, Wells JA, Christie IN, Koolen L, Abdala AP, Liu BH, Gourine AV, Teschemacher AG, Kasparov S. CNS distribution, signalling properties and central effects of G-protein coupled receptor 4. Neuropharmacology. 2018 Aug;138:381-392.